BG106734A - Pyrazolo[1,5-d][1,2,4]triazines for enhancing cognition - Google Patents
Pyrazolo[1,5-d][1,2,4]triazines for enhancing cognitionInfo
- Publication number
- BG106734A BG106734A BG106734A BG10673402A BG106734A BG 106734 A BG106734 A BG 106734A BG 106734 A BG106734 A BG 106734A BG 10673402 A BG10673402 A BG 10673402A BG 106734 A BG106734 A BG 106734A
- Authority
- BG
- Bulgaria
- Prior art keywords
- optionally substituted
- heteroaromatic ring
- alkyl
- compounds
- membered heteroaromatic
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Hospice & Palliative Care (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Psychiatry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Изобретението се отнася до съединения или до техни соли с формула, в която R1 означава халоген или С1-6 алкил, С3-7 циклоалкил, С4-7 циклоалкенил, С6-8 бициклоалкил, С6-10 арил, С3-7 хетероциклоалкил, хетероарил, или ди(С1-6)алкиламино, като всяка от тези групи може да е по избор заместена; L е О, S или NRn, където Rn е Н, С1-6 алкил или С3-6 циклоалкилалкил; W е С1-6 алкил, С2-6 алкенил или С2-6алкинил, заместени по избор; Х е NR4R5 или пет- или шестчленен хетероароматен пръстен, като пет- илишестчленният хетероароматен пръстен по избор е кондензиран към бензенов или пиридинов пръстен и хетероароматният пръстен е заместен по избор; Y е по избор разклонен С1-4 алкилен, заместен по избор с оксогрупа, или Y е група (СН2)jO, където кислородният атом е най-близкият до групата Х, j има стойност 2, 3 или 4; Z означава пет- или шестчленен хетероароматен пръстен, като който и да е от тези пръстени може да е заместен по избор. Изобретението сеотнася и до фармацевтични състави, които съдържатсъединенията, до използването им в методи за лечение и в производството на лекарства за усилване накогнитивната способност, по-специално при лечениена болестта на Алцхаймер, както и до съответнитеметоди за лечение. Съединенията са лиганди и инверсни агонисти на GABAA алфа 5 рецепторен подтип.The invention relates to compounds or to their salts of the formula wherein R1 represents halogen or C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkenyl, C6-8 bicycloalkyl, C6-10 aryl, C3-7 heterocycloalkyl, heteroaryl, or di (C 1-6) alkylamino, each of which may be optionally substituted; L is O, S or NRn, wherein R11 is H, C1-6 alkyl or C3-6 cycloalkylalkyl; W is C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl optionally substituted; X is NR4R5 or a five- or six-membered heteroaromatic ring, wherein the five- or six-membered heteroaromatic ring is optionally fused to a benzene or pyridine ring and the heteroaromatic ring is optionally substituted; Y is optionally branched C 1-4 alkylene optionally substituted with oxo, or Y is a group (CH 2) j O wherein the oxygen atom is the closest to the group X, j is 2, 3 or 4; Z represents a five- or six-membered heteroaromatic ring, any of which rings being optionally substituted. The invention also relates to pharmaceutical compositions containing the compounds, to their use in methods of treatment and in the manufacture of drugs for enhancing the cognitive ability, especially in the treatment of Alzheimer's disease, as well as to the corresponding treatment methods. The compounds are ligands and inverse agonists of the GABAA alpha 5 receptor subtype.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9927874.9A GB9927874D0 (en) | 1999-11-25 | 1999-11-25 | Therapeutic agents |
| GB0009602A GB0009602D0 (en) | 2000-04-18 | 2000-04-18 | Therapeutic agents |
| GB0018651A GB0018651D0 (en) | 2000-07-28 | 2000-07-28 | Therapeutic agents |
| PCT/GB2000/004450 WO2001038331A2 (en) | 1999-11-25 | 2000-11-22 | Pyrazolo[1,5-d][1,2,4]triazines for enhancing cognition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BG106734A true BG106734A (en) | 2003-02-28 |
Family
ID=27255677
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BG106734A BG106734A (en) | 1999-11-25 | 2002-05-22 | Pyrazolo[1,5-d][1,2,4]triazines for enhancing cognition |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US6355638B1 (en) |
| EP (1) | EP1235829A2 (en) |
| JP (1) | JP2003514909A (en) |
| KR (1) | KR20020053091A (en) |
| CN (1) | CN1391574A (en) |
| AU (1) | AU1533001A (en) |
| BG (1) | BG106734A (en) |
| BR (1) | BR0015126A (en) |
| CA (1) | CA2391103A1 (en) |
| CZ (1) | CZ20021813A3 (en) |
| EA (1) | EA200200599A1 (en) |
| EE (1) | EE200200260A (en) |
| HK (1) | HK1046406A1 (en) |
| HU (1) | HUP0203579A3 (en) |
| IL (1) | IL149051A0 (en) |
| MX (1) | MXPA02005233A (en) |
| NO (1) | NO20022456D0 (en) |
| PL (1) | PL355637A1 (en) |
| SK (1) | SK8952002A3 (en) |
| WO (1) | WO2001038331A2 (en) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0128499D0 (en) * | 2001-11-28 | 2002-01-23 | Merck Sharp & Dohme | Therapeutic agents |
| EP2298296A1 (en) | 2009-08-25 | 2011-03-23 | CNRS Centre National De La Recherche Scientifique | Composition and method for treating cognitive impairments in down syndrome subjects |
| NZ705135A (en) * | 2010-05-26 | 2017-10-27 | Sunovion Pharmaceuticals Inc | Heteroaryl compounds and methods of use thereof |
| US20150374705A1 (en) * | 2012-02-14 | 2015-12-31 | Shanghai Institues for Biological Sciences | Substances for treatment or relief of pain |
| CN107344938B (en) * | 2016-05-06 | 2022-05-06 | 上海赛默罗生物科技有限公司 | Pyrazole-triazine derivative, preparation method thereof, pharmaceutical composition and application thereof |
| CN107344936B (en) * | 2016-05-06 | 2022-06-03 | 上海赛默罗生物科技有限公司 | Triazolopyridazine derivative, preparation method, pharmaceutical composition and application thereof |
| CN114258390A (en) * | 2019-06-19 | 2022-03-29 | 生物马林药物股份有限公司 | Glycolate oxidase inhibitors for disease treatment |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL331072A1 (en) * | 1996-07-25 | 1999-06-21 | Merck Sharp & Dohme | Substututed derivatives of triazolo-pyrydazine as ligands for gaba receptors |
| GB9715977D0 (en) * | 1997-07-29 | 1997-10-01 | Merck Sharp & Dohme | Therapeutic agents |
| AU746866B2 (en) * | 1998-01-14 | 2002-05-02 | Merck Sharp & Dohme Limited | Triazolo-pyridazine derivatives as ligands for GABA receptors |
| GB9806102D0 (en) * | 1998-03-20 | 1998-05-20 | Merck Sharp & Dohme | Therapeutic agents |
| US6479506B1 (en) * | 1998-06-16 | 2002-11-12 | Merck Sharp & Dohme Ltd. | Triazolo-pyridine derivatives as ligands for GABA receptors |
| CA2346289A1 (en) * | 1998-10-16 | 2000-04-27 | Merck Sharp & Dohme Limited | Pyrazolo-triazine derivatives as ligands for gaba receptors |
-
2000
- 2000-11-21 US US09/717,423 patent/US6355638B1/en not_active Expired - Lifetime
- 2000-11-22 EA EA200200599A patent/EA200200599A1/en unknown
- 2000-11-22 CZ CZ20021813A patent/CZ20021813A3/en unknown
- 2000-11-22 PL PL00355637A patent/PL355637A1/en not_active Application Discontinuation
- 2000-11-22 WO PCT/GB2000/004450 patent/WO2001038331A2/en not_active Application Discontinuation
- 2000-11-22 IL IL14905100A patent/IL149051A0/en unknown
- 2000-11-22 SK SK895-2002A patent/SK8952002A3/en unknown
- 2000-11-22 JP JP2001540094A patent/JP2003514909A/en not_active Withdrawn
- 2000-11-22 KR KR1020027006672A patent/KR20020053091A/en not_active Application Discontinuation
- 2000-11-22 BR BR0015126-2A patent/BR0015126A/en not_active Application Discontinuation
- 2000-11-22 EP EP00977692A patent/EP1235829A2/en not_active Withdrawn
- 2000-11-22 MX MXPA02005233A patent/MXPA02005233A/en not_active Application Discontinuation
- 2000-11-22 HU HU0203579A patent/HUP0203579A3/en unknown
- 2000-11-22 AU AU15330/01A patent/AU1533001A/en not_active Abandoned
- 2000-11-22 CN CN00816013A patent/CN1391574A/en active Pending
- 2000-11-22 CA CA002391103A patent/CA2391103A1/en not_active Abandoned
- 2000-11-22 EE EEP200200260A patent/EE200200260A/en unknown
-
2002
- 2002-05-22 BG BG106734A patent/BG106734A/en unknown
- 2002-05-24 NO NO20022456A patent/NO20022456D0/en not_active Application Discontinuation
- 2002-10-29 HK HK02107821.8A patent/HK1046406A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| NO20022456L (en) | 2002-05-24 |
| JP2003514909A (en) | 2003-04-22 |
| MXPA02005233A (en) | 2002-11-07 |
| CN1391574A (en) | 2003-01-15 |
| SK8952002A3 (en) | 2002-10-08 |
| BR0015126A (en) | 2002-07-02 |
| CZ20021813A3 (en) | 2002-08-14 |
| EE200200260A (en) | 2003-06-16 |
| EP1235829A2 (en) | 2002-09-04 |
| AU1533001A (en) | 2001-06-04 |
| WO2001038331A3 (en) | 2001-11-08 |
| CA2391103A1 (en) | 2001-05-31 |
| IL149051A0 (en) | 2002-11-10 |
| HUP0203579A3 (en) | 2003-07-28 |
| PL355637A1 (en) | 2004-05-04 |
| NO20022456D0 (en) | 2002-05-24 |
| HK1046406A1 (en) | 2003-01-10 |
| HUP0203579A2 (en) | 2003-03-28 |
| WO2001038331A2 (en) | 2001-05-31 |
| EA200200599A1 (en) | 2002-12-26 |
| KR20020053091A (en) | 2002-07-04 |
| US6355638B1 (en) | 2002-03-12 |
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